Dual Inhibitor of mPGES-1 and 5-LO
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CAY10589

Item No. 13164

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[4-[([1,1’-biphenyl]-4-ylmethyl)amino]-6-chloro-2-pyrimidinyl]thio]-octanoic acid
CAS Number
1077626-52-8
Molecular Formula
C25H28ClN3O2S
Formula Weight
470.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
254 nm
SMILES
ClC1=CC(NCC2=CC=C(C3=CC=CC=C3)C=C2)=NC(SC(C(O)=O)CCCCCC)=N1
InChi Code
InChI=1S/C25H28ClN3O2S/c1-2-3-4-8-11-21(24(30)31)32-25-28-22(26)16-23(29-25)27-17-18-12-14-20(15-13-18)19-9-6-5-7-10-19/h5-7,9-10,12-16,21H,2-4,8,11,17H2,1H3,(H,30,31)(H,27,28,29)
InChi Key
FQMPYBCEABTPIK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $61

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    5 mg

    $260

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    10 mg

    $462

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    Product Description

    Microsomal Prostaglandin E2 Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC50 = 1.3 μM) and 5-LO (IC50 = 1.0 μM).1 It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Koeberle, A., Zettl, H., Greiner, C., et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J. Med. Chem. 51(24), 8068-8076 (2008).